EP 1745071 B1 20140312 - MSH-AGONIST TRIPEPTIDE CONJUGATES
Title (en)
MSH-AGONIST TRIPEPTIDE CONJUGATES
Title (de)
TRIPEPTIDKONJUGATE ALS MSH-AGONISTEN
Title (fr)
CONJUGUES TRIPEPTIDIQUES AGONISTES DE LA MSH
Publication
Application
Priority
- FR 2005001165 W 20050510
- FR 0405069 A 20040511
- FR 0411276 A 20041022
Abstract (en)
[origin: WO2005116067A2] The invention relates to a tripeptide conjugate having general formula I, A-AA1-AA2-AA3-NH2, wherein A represents the radical corresponding to a monocarboxylic acid with general formula II, HOOC-R, in which: R represents a linear or branched aliphatic radical at C1-C24, which is optionally substituted by a hydroxyl group and which can comprise one or more unsaturations, preferably between 1 and 6 unsaturations, lipoic acid or the reduced form thereof, dihydrolipoic acid, N- lipoyllysine, or phenylbutyric acid; and AA1, AA2 and AA3, which may be identical or different, represent independently of each other an amino acid selected from His, Phe, Ala, Arg, Lys, Orn, Trp, Nap, Tpi and Tic, on the condition that at least one of AA1, AA2 or AA3 represent Phe, preferably Dphe in the form of enantiomers or diastereoisomers and mixtures thereof, including racemic mixtures.
IPC 8 full level
A61K 47/48 (2006.01); A61K 38/06 (2006.01); A61K 38/34 (2006.01); A61P 17/00 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 37/00 (2006.01); A61Q 17/04 (2006.01); C07K 5/08 (2006.01); C07K 5/097 (2006.01); C07K 7/04 (2006.01); C07K 14/685 (2006.01)
CPC (source: EP US)
A61K 47/542 (2017.07 - EP US); A61P 3/04 (2017.12 - EP); A61P 11/06 (2017.12 - EP); A61P 17/00 (2017.12 - EP); A61P 17/02 (2017.12 - EP); A61P 17/04 (2017.12 - EP); A61P 17/06 (2017.12 - EP); A61P 17/16 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 35/00 (2017.12 - EP); A61P 37/00 (2017.12 - EP); A61P 37/08 (2017.12 - EP)
Citation (examination)
- KOIKOV L N ET AL: "Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH2) 3CO-His-D-Phe-Arg-Trp-NH2]. An additional binding site within the human melanocortin receptor 1?", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS 20040802 GB LNKD- DOI:10.1016/J.BMCL.2004.05.039, vol. 14, no. 15, 2 August 2004 (2004-08-02), pages 3997 - 4000, ISSN: 0960-894X
- KOIKOV L.N. ET AL: "Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Tryp-NH2", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 13, 2003, pages 2647 - 2650, XP002342336
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 2005116067 A2 20051208; WO 2005116067 A3 20060608; CA 2565805 A1 20051208; EP 1745071 A2 20070124; EP 1745071 B1 20140312; ES 2456090 T3 20140421; FR 2870243 A1 20051118; FR 2870243 B1 20101119; JP 2008502599 A 20080131; JP 4897970 B2 20120314; US 8017581 B1 20110913
DOCDB simple family (application)
FR 2005001165 W 20050510; CA 2565805 A 20050510; EP 05770969 A 20050510; ES 05770969 T 20050510; FR 0411276 A 20041022; JP 2007512281 A 20050510; US 59604105 A 20050510